Microbial metabolites of harman alkaloids.

abstract：:A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

更新日期：1996-11-01 00:00:00

abstract：:The metabolism of 2,4-dinitrotoluene (2,4-DNT), 2,4-dinitrobenzyl alcohol (2,4-DNB), 2,4-dinitrobenzaldehyde (2,4-DNBAl), 2,6-DNT, 2,6-DNB and 2,6-DNBAl in the microsomal and cytosol fractions prepared from unfortified male Wistar and male Sprague-Dawley (S.D.) rat livers was investigated. Data obtained by high-perfor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori M,Kawajiri T,Sayama M,Miyahara T,Kozuka H

更新日期：1989-07-01 00:00:00

abstract：:A novel fucan sulfate (Hor-1) was isolated from the hot water extract of an edible brown alga, Sargassum horneri (Turner) C. Agardh. The fucan sulfate was revealed to have sugar linkage types, sulfate content and uronic acid content different from those of sodium hornan (Na-HOR), another fucan sulfate isolated from th...

journal_title：Chemical & pharmaceutical bulletin

authors： Preeprame S,Hayashi K,Lee JB,Sankawa U,Hayashi T

更新日期：2001-04-01 00:00:00

abstract：:A novel method for thermodynamic stability studies of polymorphic drug substances has been developed. In order to estimate the transition temperature for an enantiotropic polymorphic pair, a formula for calculating the temperature at which the solubilities of each polymorph become equal has been derived with heat of s...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Shono Y,Higashi A,Umemoto K,Godo M

更新日期：2002-02-01 00:00:00

abstract：:As the glycosyl constituents of Ficus pumila L. fruits (Moraceae), three new sesquiterpenoid glucosides, pumilasides A, B and C were isolated together with benzyl beta-D-glucopyranoside, (E)-2-methyl-2-butenyl beta-D-glucopyranoside and rutin. Their structures were characterized as (1S,4S,5R,6R,7S,10S)-1,4,6-trihydrox...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima J,Kimizuka K,Tanaka Y

更新日期：2000-01-01 00:00:00

abstract：:The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hiroya K,Takahashi T,Shimomae K,Sakamoto T

更新日期：2005-02-01 00:00:00

abstract：:A novel C-methylated biflavone, taiwanhomoflavone-B (1), together with known compounds, 7,4',7"-tri-O-methylamentoflavone, 6-C-methylnaringenin and apigenin-7-O-beta-glucoside were isolated from an ethanolic extract of Cephalotaxus wilsoniana. The structure of 1 was elucidated on the basis of spectroscopic analysis. T...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Hwang SY,Yang Kuo LM,Lee YL,Li SY,Shen YC

更新日期：2002-12-01 00:00:00

abstract：:Optically active structural isomers (1b-f and dst-1b-f) of 3',4'-di-(O)-(-)-camphanoyl-(+)-khellactone (DCK) were synthesized and their anti-human immunodeficiency virus (HIV) activity was investigated. The value of the sensitivity index (SI) of 1b was greater than that of DCK. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishioka H,Uesugi K,Ueda N,Kondo Y,Tsuji M,Abe H,Harayama T,Hamasaki T,Baba M,Takeuchi Y

更新日期：2011-01-01 00:00:00

abstract：:The purpose of this research is to investigate the applicability of terahertz (THz) reflectance spectroscopy for quantification of drug substance in tablets, so as to demonstrate the feasibility for applying this technique to tableting process monitoring. In order to acquire a suitable absorbance spectrum for this pur...

journal_title：Chemical & pharmaceutical bulletin

authors： Hisazumi J,Watanabe T,Suzuki T,Wakiyama N,Terada K

更新日期：2012-01-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 00:00:00

abstract：:The influence of various phenolic compounds on the lactoperoxidase (LPO)/hydrogen peroxide (H2O2)-catalyzed oxidation of biochemical reductants such as reduced beta-nicotinamide adenine dinucleotide (NADH), reduced beta-nicotinamide adenine dinucleotide phosphate (NADPH) or reduced glutathione (GSH) was investigated b...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda J,Tsuchiya Y,Ozawa T

更新日期：2001-03-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

更新日期：2005-12-01 00:00:00

abstract：:In this study, two novel complexes [Cu(MCVH)phen(H(2)O)].ClO(4) (1) and [Cu(MCLH)phen(H(2)O)].ClO(4) (2) (here, MCVH(2)=(7-hydroxy-4-methyl-8-coumarinyl) valine, MCLH(2)=(7-hydroxy-4-methyl-8-coumarinyl) leucine) have been synthesized and characterized by elemental analyses, molar conductance, infrared spectra (IR), (...

journal_title：Chemical & pharmaceutical bulletin

authors： Jia L,Xu XM,Xu J,Chen LH,Jiang P,Cheng FX,Lu GN,Wang Q,Wu JC,Tang N

更新日期：2010-08-01 00:00:00

abstract：:The oxidative behaviour of, a hypnotic drug, zolpidem was studied at glassy carbon electrode in Britton-Robinson buffer over the pH range 2.0-11.0 using cyclic, linear sweep and differential pulse voltammetry. Oxidation of the drug was effected in a single irreversible, diffusion-controlled step. Using differential pu...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Bekhiet G,Wahdan T

更新日期：2004-09-01 00:00:00

abstract：:Three new natural sesquiterpene coumarins, isofeterin (1), lehmannolol (3), sinkianone (4), and one known compound, lehmannolone (2), were isolated from the roots of Ferula teterrima and Ferula sinkiangensis. Their chemical structures were established on the basis of spectroscopic analysis, including X-ray crystallogr...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang JR,An Z,Li ZH,Jing S,Qina HL

更新日期：2006-11-01 00:00:00

abstract：:Oiling-out is a unique phenomenon that the liquid phase is separated into two parts during crystallization. The emergence of new liquid phase changes the environment where crystals nucleate and grow, we call "mother phase," because target material and impurities become distributed to each phase according to their own ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Takiyama H

更新日期：2020-01-01 00:00:00

abstract：:The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were ch...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishii H,Yamaguchi K,Seki H,Sakamoto S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-08-01 00:00:00

abstract：:Two novel norhumulene-type sesquiterpenes, named mikaniahumulene I (1) and II (2) were isolated along with nine known compounds, seven kaurenic acid-type diterpenes (3-9), a coumarin (10) and a flavone (11), from the aerial parts of Mikania hirsutissima DC (Compositae). The structures of new norhumulenes were determin...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkoshi E,Makino M,Fujimoto Y

更新日期：1999-10-01 00:00:00

abstract：:Four new dibenzocyclooctadiene lignan glucosides, schisandrosides A-D (1-4), as well as two known rare nortriterpenoids, micrandilactone C (5) and propindilactone Q (6), were isolated from the roots of Schisandra chinensis BAILLON (Schisandraceae). The structure of compounds 1-4 were elucidated by physical and spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim HM,Ryu B,Lee JS,Choi JH,Jang DS

更新日期：2015-01-01 00:00:00

abstract：:Seventeen saponins isolated from the root of Pulsatilla koreana were examined for their in vitro cytotoxic activity against the human solid cancer cell lines, A-549, SK-OV-3, SK-MEL-2, and HCT15, using the SRB assay method, and their in vivo antitumor activity using BDF1 mice bearing Lewis lung carcinoma (LLC). The sa...

journal_title：Chemical & pharmaceutical bulletin

authors： Bang SC,Lee JH,Song GY,Kim DH,Yoon MY,Ahn BZ

更新日期：2005-11-01 00:00:00

abstract：:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-ben...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyadera A,Satoh K,Imura A

更新日期：2000-04-01 00:00:00

abstract：:A series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalcemia model in rats (PIH model). Among these compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi M,Sakamoto S,Yoshida M,Abe T,Isomura Y

更新日期：1993-04-01 00:00:00

abstract：:The purpose of this study was to develop and test a novel and simple method for evaluating the disintegration time of rapidly disintegrating tablets (RDTs) in vitro, since the conventional disintegration test described in the pharmacopoeia produces poor results due to the difference of its environmental conditions fro...

journal_title：Chemical & pharmaceutical bulletin

authors： Hoashi Y,Tozuka Y,Takeuchi H

更新日期：2013-01-01 00:00:00

abstract：:Electrochemical oxidation of catechols in the presence of phenyl-Meldrum's acid as a nucleophile in aqueous solution has been studied in detail by means of cyclic voltammetry and controlled potential coulometry. The results indicate that the o-benzoquinone derived from catechols participates in Michael addition reacti...

journal_title：Chemical & pharmaceutical bulletin

authors： Nematollahi D,Bamzadeh M,Shayani-Jam H

更新日期：2010-01-01 00:00:00

abstract：:A series of N-substituted 3,4-diphenyl-1H-pyrrole-2,5-diones (diphenylmaleimides) (IV) were synthesized and tested for cytostatic activity. Compounds IVa--k were prepared from diphenylmaleic anhydride or its dinitro derivative (V or VI) and the corresponding amine. Compounds IVl--n were obtained by reaction of 3-(p-ni...

journal_title：Chemical & pharmaceutical bulletin

authors： Fernández Braña M,Fernández A,Garrido M,López Rodríguez ML,Morcillo MJ,Sanz AM

更新日期：1989-10-01 00:00:00

abstract：:In order to synthesize four stereoisomers of cystathionine (CYT), D- and L-homocysteines (D- and L-Hcy) were synthesized from methionine (Met) by a facile procedure. L-Met was reacted with dichloroacetic acid in concentrated hydrochloric acid under reflux to give (4S)-1,3-thiazane-2,4-dicarboxylic acid hydrochloride [...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Nakagawa K,Kanemoto N,Kinda T,Yamamoto H

更新日期：2002-08-01 00:00:00

abstract：:Oral gel formulations are known as easy to administer drug products for patients who have problems taking drugs including those with conditions such as dysphagia. In addition, there are numerous commercially available oral gel products, most of which are immediate-release formulation that release their pharmaceutical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hishikawa Y,Kakino Y,Tsukamoto H,Tahara K,Onodera R,Takeuchi H

更新日期：2016-01-01 00:00:00

abstract：:The superoxide O2(·-) scavenging reaction of (+)-catechin (Cat), quercetin (Que), rutin, and α-tocopherol (α-TOH) as natural phenolic compounds is investigated on the basis of electrochemical and ESR spectral measurements with the aid of density functional theory (DFT) calculations. Reversibility of the O2/O2(·-) redo...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama T,Uno B

更新日期：2015-01-01 00:00:00